海洋疣荔枝螺体外抗肿瘤活性

摘要

Rock shells,Thais clavigera,as one of the most popular seafood in Fujian Province,are proved to have pharmaceutical activities according to the traditional Chinese medicine records and the historical usage.However, there are few public reports about the active components from the snail.In this paper,we isolated and screened the anti-tumor substances E-EA-2 from the rock shells.The main component of E-EA-2 was identified as 6-bromoisat-ine by means of HPLC and GC-MS.The cancer cell proliferations (MCF-7 and QGY-7703)were significantly in-hibited when the concentration of E-EA-2 exceeded 40 μg/cm3 .E-EA-2 could induce PARP cleavage in QGY-7703 cells.While the number of survival cancer cells obviously increased at presence of cell permeable pan caspase inhibitor Z-VAD.And cultured MCF-7 cells with E-EA-2 after 24h,cell nuclear shrinkage,loss of mitochondrial membrane potential and cell apoptosis were obvious.The IC50 of E-EA-2 was 46 μg/cm3 and 28 μg/cm3 to QGY-7703 and MCF-7,respectively.The anti-tumor effects of E-EA-2 might be taken through promoting cell apoptosis.%荔枝螺是福建海域常见食用螺类，古方记载和民间长期食用证实具有良好药用价值，但国内外对其生物活性物质的研究还较少．本研究以福建海域疣荔枝螺（Thais clavigera）为研究材料，从疣荔枝螺消化腺部位获得抗癌组分E-EA-2，通过液相色谱、气质联用色谱分析发现其主要成分为6-溴靛红（6-bromoisatine），分子结构式C8 H4 BrNO2．E-EA-2能有效抑制人乳腺癌MCF-7、人肝癌QGY-7703细胞增殖，药物浓度高于40μg／cm3时，癌细胞存活率显著降低．E-EA-2能诱导肝癌细胞QGY-7703发生PARP蛋白剪切，加入泛caspase 抑制剂使细胞存活率显著提高．同时，E-EA-2使MCF-7细胞核产生固缩，线粒体膜电位显著下降，凋亡细胞数量显著增加．E-EA-2对肝癌细胞QGY-7703的IC50为46μg／cm3，对乳腺癌细胞MCF-7的IC50为28μg／cm3，对癌细胞的增殖抑制作用主要是以促凋亡方式实现的．